[Synthesis, structure elucidation and biological activity of thio- analogs of drugs with the examples of chlorthenoxazine and amobarbital].
Two drugs (chlorthenoxazine, amobarbital) were converted into their S-analogues derivatives via thiation with the P4S10-pyridine complex. The identity of structure isomers was confirmed by 13C NMR. A preliminary evaluation for their biological activities revealed that trithioamobarbital exhibits some notable spasmolytic effects. The substitution of oxygen by sulphur in chlorthenoxazine resulted in a complete loss of antiinflammatory activity.
Stratmann
J
J
Institut für Pharmazie, Johannes Gutenberg-Universität Mainz.
D000654:Amobarbital / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D000700:Analgesics / Q000138:chemical synthesis / Q000494:pharmacology; D000818:Animals; D048588:Benzoxazines; D009682:Magnetic Resonance Spectroscopy; D051379:Mice; D010078:Oxazines / Q000138:chemical synthesis / Q000494:pharmacology*; D010276:Parasympatholytics / Q000138:chemical synthesis; D011930:Reaction Time
D000700:Analgesics; D048588:Benzoxazines; D010078:Oxazines; D010276:Parasympatholytics; C007032:chlorthenoxazin; D000654:Amobarbital
Synthese, Strukturaufklärung und biologische Wirksamkeitsprüfung thioanaloger Arzneistoffe am Beispiel des Chlorthenoxazins und Amobarbitals.